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Kynurenic acid sodium is an endogenous tryptophan metabolite with activity against NMDA, glutamate, α7 nicotinic acetylcholine receptors. Also acting as an agonist of GPR35/CXCR8.
| ln Vitro |
GPR35 is a receptor for kynurenic acid, an intermediary in the kynurenine process. In the presence of G qi/o chimeric G proteins, kynurenic acid causes calcium mobilization and inositol phosphate synthesis in a manner that is dependent on GPR35. In GPR35-expressing cells, kynurenic acid increases [35S]guanosine 5′-O-(3-thiotriphosphate) binding; treatment with pertussis toxin reverses this effect. Moreover, kynurenic acid causes GPR35 to internalize[1]. The neuroprotective, anticonvulsant, and neuroinhibitory properties of KYNA are seen at millimolar concentrations of the molecule. The observation that KYNA concentrations in the mammalian brain are in the sub-micromolar range, coupled with the low affinity of KYNA at each of the three ionotropic glutamate receptors responsible for these effects (NMDA, alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), and kainate), suggested that other receptors might be targets of endogenous kynurenic acid. With an IC50 in the low micromolar range, kynurenic acid antagonizes α7nAChRs on cultured hippocampus neurons non-competitively and with a steeper inhibition curve[2].
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| ln Vivo |
Leukocyte activity in the peripheral blood of mice is influenced by kynurenic acid; however, the most significant effect is produced by the lowest concentration (2.5 mg/L) and the maximum concentration (250 mg/L) has the least effect. After 7 and 28 days, an animal's T lymphocyte proliferative response is stimulated (p<0.05) by a dosage of kynurenic acid[3].
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| References |
[1]. Wang J, et al. Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. J Biol Chem. 2006 Aug 4;281(31):22021-8.
[2]. Albuquerque EX, et al. Kynurenic acid as an antagonist of α7 nicotinic acetylcholine receptors in the brain: facts and challenges. Biochem Pharmacol. 2013 Apr 15;85(8):1027-32. [3]. Małaczewska J, et al. Effect of oral administration of kynurenic acid on the activity of the peripheral blood leukocytes in mice. Cent Eur J Immunol. 2014;39(1):6-1 |
| Molecular Formula |
C10H6NNAO3
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| Molecular Weight |
211.14931344986
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| CAS # |
2439-02-3
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| Related CAS # |
Kynurenic acid;492-27-3
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| SMILES |
[Na+].O=C1C=C(C(=O)[O-])NC2C=CC=CC=21
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~236.80 mM)
H2O : ~0.1 mg/mL (~0.47 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7360 mL | 23.6798 mL | 47.3597 mL | |
| 5 mM | 0.9472 mL | 4.7360 mL | 9.4719 mL | |
| 10 mM | 0.4736 mL | 2.3680 mL | 4.7360 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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